2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. Btk

Btk

Bruton tyrosine kinase

Btk

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Bruton tyrosine kinase (Btk) is a member of the Tec family kinases with a well-characterized role in B-cell antigen receptor (BCR)-signaling and B-cell activation.

Btk plays a crucial role in B cell development and activation through the BCR signaling pathway and represents a new target for diseases characterized by inappropriate B cell activity. Btk is a kinase expressed exclusively in B cells and myeloid cells and has a well characterized, vital role in B cells highlighted by the human primary immune deficiency disease, X-linked agammaglobulinemia (XLA), which results from mutation in the Btk gene. Btk plays an essential role in the BCR signaling pathway. Antigen binding to the BCR results in B cell receptor oligomerization, Syk and Lyn kinase activation, followed by Btk kinase activation. Once activated, Btk forms a signaling complex with proteins such as BLNK, Lyn, and Syk and phosphorylates phospholipase C (PLC)γ2. This leads to downstream release of intracellular Ca2+ stores and propagation of the BCR signaling pathway through extracellular signal-regulated kinase and NF-κB signaling, ultimately resulting in transcriptional changes to foster B cell survival, proliferation, and/or differentiation.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15805
    KIN-8194
    		Inhibitor 98.01%
    KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC50 values of 0.915 and <0.495 nM, respectively. KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma (MCL). KIN-8194 overcomes ibrutinib (HY-10997) resistance with a survival benefit in TMD-8 ABC DLBCL xenografted mice.
    KIN-8194
  • HY-17600S
    Acalabrutinib-d4
    		Inhibitor 99.50%
    Acalabrutinib-d4 is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor[1]. Acalabrutinib-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Acalabrutinib-d<sub>4</sub>
  • HY-135334
    ACP-5862
    		Inhibitor 98.41%
    ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM.
    ACP-5862
  • HY-101474B
    (R)-Zanubrutinib
    		98.97%
    (R)-Zanubrutinib is the R enantiomer of Zanubrutinib (HY-101474A). (R)-Zanubrutinib inhibits Bruton's tyrosine kinase (Btk) with an IC50 of 11 nM.
    (R)-Zanubrutinib
  • HY-132879
    TAK-020
    		Inhibitor 99.93%
    TAK-020 is a covalent Btk inhibitor, which becomes the clinical candidate.
    TAK-020
  • HY-132808
    Atuzabrutinib
    		Inhibitor 98.01%
    Atuzabrutinib (SAR 444727) is a potent, selective reversible inhibitor of Btk (Bruton's tyrosine kinase) inhibitor. Atuzabrutinib inhibits neutrophil recruitment via inhibition of macrophage antigen-1 signalling.
    Atuzabrutinib
  • HY-122830
    DD-03-171
    		Degrader 98.72%
    DD-03-171 is a BTK PROTAC degrader, the BTK IC50 a value of 5.1 nM. DD-03-171 has an antiproliferative effect on mantle cell lymphoma (MCL) cells. (Pink: BTK inhibitor (HY-168292); Black: linker (HY-28875); Blue: CRBN Ligand (HY-131717))
    DD-03-171
  • HY-101766
    Btk inhibitor 2
    		Inhibitor 99.57%
    Btk inhibitor 2 (BGB-3111 analog) is a Bruton's tyrosine kinase (BTK) inhibitor extracted from patent US 20170224688 A1.
    Btk inhibitor 2
  • HY-131705
    BTK inhibitor 17
    		Inhibitor 99.53%
    BTK inhibitor 17 is a potent and orally active irreversible BTK inhibitor with an IC50 of 2.1 nM. BTK inhibitor 17 can be used for rheumatoid arthritis research.
    BTK inhibitor 17
  • HY-101793
    BMS-935177
    		Inhibitor 99.11%
    BMS-935177 is a potent and selective reversible inhibitor of Bruton’s tyrosine kinase (Btk) with an IC50 of 3 nM.
    BMS-935177
  • HY-100659
    Dihydrodiol-Ibrutinib
    		Inhibitor 99.92%
    Dihydrodiol-Ibrutinib (PCI-45227) is a dihydrodiol active metabolite of Ibrutinib (HY-10997), has inhibitory activity towards BTK approximately 15 times lower than that of ibrutinib.
    Dihydrodiol-Ibrutinib
  • HY-147943
    PROTAC BTK Degrader-1
    		98.87%
    PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth. PROTAC BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PROTAC BTK Degrader-1
  • HY-101474S
    Zanubrutinib-d5
    		Inhibitor ≥99.0%
    Zanubrutinib-d5 is deuterium labeled Zanubrutinib. Zanubrutinib is a selective Bruton tyrosine kinase (Btk) inhibitor[1].
    Zanubrutinib-d<sub>5</sub>
  • HY-163565
    BIIB129
    		Inhibitor 99.54%
    BIIB129 is a covalent, selective, small molecule inhibitor of Bruton's tyrosine kinase (BTK) capable of penetrating the blood-brain barrier. BIIB129 inhibits the activity of BTK by covalently binding to Cys481 in BTK, thereby affecting the function of B cells and myeloid cells. BIIB129 can be used in multiple sclerosis (MS) research.
    BIIB129
  • HY-160141
    BTK-IN-29
    		Inhibitor
    BTK-IN-29 (compound 14) is an inhibitor of Btk.
    BTK-IN-29
  • HY-15427A
    GDC-0834 Racemate
    		98.04%
    GDC-0834 Racemate is the racemate form of GDC-0834, which is a potent and selective BTK inhibitor with in vitro IC50s of 5.
    GDC-0834 Racemate
  • HY-125997
    BTK inhibitor 10
    		Inhibitor 99.66%
    BTK inhibitor 10 is a potent and orally active Bruton kinase (BTK) inhibitor, extracted from patent WO2018145525, example 33. BTK inhibitor 10 has a potential for rheumatoid arthritis treatment.
    BTK inhibitor 10
  • HY-136531
    XMU-MP-3
    		Inhibitor 98.27%
    XMU-MP-3 is a potent non-covalent BTK inhibitor with IC50s of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation in the presence of 10 μM ATP, respectively. XMU-MP-3 also induces apoptosis.
    XMU-MP-3
  • HY-15427B
    GDC-0834 (S-enantiomer)
    		98.03%
    GDC-0834 (S-enantiomer) is the S-enantiomer of GDC-0834. GDC-0834 is a potent and selective BTK inhibitor.
    GDC-0834 (S-enantiomer)
  • HY-153220A
    (R)-NX-2127
    		Degrader
    (R)-NX-2127 ((R)-compound 28) is an isomer of the BTK PROTAC degrader NX-2127 (HY-153220). (R)-NX-2127 is composed of PROTAC target protein ligand (red part) BTK ligand 10 (HY-168302), E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383) and PROTAC Linker (black part) Thalidomide-pyrrolidine-C-piperidine-Ph-NH2 (HY-168304).
    (R)-NX-2127
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity